Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the pediatric preclinical testing program1. Issue 7 (9th January 2013)

• Record Type: Journal Article
• Authors: Lock, Richard B.; Carol, Hernan; Maris, John M.; Kang, Min H.; Reynolds, C. Patrick; Kolb, E. Anders; Gorlick, Richard; Keir, Stephen T.; Billups, Catherine A.; Kurmasheva, Raushan T.; Houghton, Peter J.; Smith, Malcolm A.
• Is Part Of: Pediatric blood & cancer. Volume 60:Issue 7(2013:Jul.)
• Page Start: E42
• Page End: E45
• Publication Date: 2013-01-09
• Subjects: Tumors in children -- Periodicals; Blood -- Diseases -- Periodicals; Cancer in children -- Periodicals; 618.92
• DOI: 10.1002/pbc.24451
• Languages: English
• ISSNs: 1545-5009

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>Ganetespib, an Hsp90 inhibitor, was tested against the PPTP <italic>in vitro</italic> cell line panel and selected xenografts <italic>in vivo</italic>, including JAK2‐ and BRAF‐mutated models. Ganetespib demonstrated potent <italic>in vitro</italic> cytotoxic activity (median rIC₅₀ 8.8 nM, range 4.4–27.1 nM). <italic>In vivo</italic>, ganetespib induced significant differences in EFS distribution for 4 of 11 xenografts. Intermediate activity (EFS T/C &gt; 2) was noted only for the MV4;11 xenograft, and there were no objective responses. Administered as single agents, Hsp90 inhibitors examined by the PPTP have shown limited evidence for a therapeutic window against both solid tumor and leukemia pediatric preclinical models. Pediatr Blood Cancer 2013; 60: E42–E45. © 2013 Wiley Periodicals, Inc.</p> </abstract>